US8895695B2ExpiredUtilityA1
Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity

Assignee: ZUMBRUNN JÜRGPriority: May 2, 2003Filed: Jul 1, 2010Granted: Nov 25, 2014
Est. expiryMay 2, 2023(expired)· nominal 20-yr term from priority
Inventors:Jürg Zumbrunn Steven J. Demarco Sergio Lociuro Jan Wim Vrijbloed Frank Gombert Reshmi Mukherjee Kerstin Moehle Daniel Obrecht John Anthony Robinson Heiko Henze Barbara Romagnoli Christian Ludin
A61P 35/00A61P 37/04A61P 31/12A61P 35/04A61P 43/00A61P 31/18A61P 29/00C07K 1/047C07K 7/64A61K 38/00A61K 38/12A61K 38/10C07K 7/08C07K 1/04
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Claims
Abstract

Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1. A compound of the general formula 
       
         
           
           
               
               
           
         
         wherein 
       
       
         
           
           
               
               
           
         
         is a group of one of the formulae 
       
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         is Gly or the residue of an L-α-amino acid with B being a residue of formula —NR 20 CH(R 71 )— or the enantiomer of one of the groups A1 to A69 as defined hereinafter; 
       
       
         
           
           
               
               
           
         
         is a group of one of the formulae 
       
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         R 1  is H; lower alkyl; or aryl-lower alkyl; 
         R 2  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 3  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 4  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s SR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) p (CHR 61 ) s COOR 57 ; —(CH 2 ) p (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) p CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 5  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 6  is H; alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 7  is alkyl; alkenyl; —(CH 2 ) q (CHR 61 ) s OR 55 ; —(CH 2 ) q (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) q (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) q (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) r (CHR 61 ) s COOR 57 ; —(CH 2 ) r (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) r CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) r (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) r (CHR 61 ) s C 6 H 4 R 8 ; 
         R 8  is H; Cl; F; CF 3 ; NO 2 ; lower alkyl; lower alkenyl; aryl; aryl-lower alkyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 )NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s COR 64 ; 
         R 9  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 10  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 11  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 12  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) r (CHR 61 ) s COOR 57 ; —(CH 2 ) r (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) r (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2   r (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) r (CHR 61 ) s C 6 H 4 R 8 ; 
         R 13  is alkyl; alkenyl; —(CH 2 ) q (CHR 61 ) s OR 55 ; —(CH 2 ) q (CHR 61 ) s SR 56 ; —(CH) q (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) q (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) q (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) q (CHR 61 ) s COOR 57 ; —(CH 2 ) q (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) q CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) q (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) q (CHR 61 ) s C 6 H 4 R 8 ; 
         R 14  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —m(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) q (CHR 61 ) s COOR 57 ; —(CH 2 ) q (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) q CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) q (CHR 61 ) s SOR 62 ; or —(CH 2 ) q (CHR 61 ) s C 6 H 4 R 8 ; 
         R 15  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 16  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 17  is alkyl; alkenyl; —(CH 2 ) q (CHR 61 ) s OR 55 ; —(CH 2 ) q (CHR 61 ) s SR 56 ; —(CH) q (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) q (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) q (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) q (CHR 61 ) s COOR 57 ; —(CH 2 ) q (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) q CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) q (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) q (CHR 61 ) s C 6 H 4 R 8 ; 
         R 18  is alkyl; alkenyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 61 ) s SR 56 ; —(CH) p (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) p (CHR 61 ) s COOR 57 ; —(CH 2 ) p (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) p (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 19  is lower alkyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 61 ) s SR 56 ; —(CH 2   p (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR61) s NR 20 CONR 33 R 82 ; —(CH 2 ) p (CHR 61 ) s COOR 57 ; —(CH 2 ) p (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) p CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; or 
         R 18  and R 19  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 (CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 20  is H; alkyl; alkenyl; or aryl-lower alkyl; 
         R 21  is H; alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 22  is H; alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s R 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o )CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 23  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 24  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 25  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 26  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; or 
         R 25  and R 26  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) r O(CH 2 ) r —; —(CH 2 ) r S(CH 2 ) r —; or —(CH 2 ) r NR 57 (CH 2 ) r —; 
         R 27  is H; alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 28  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s —OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 29  is alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —(CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 30  is H; alkyl; alkenyl; or aryl-lower alkyl; 
         R 31  is H; alkyl; alkenyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 32  is H; lower alkyl; or aryl-lower alkyl; 
         R 33  is H; alkyl, alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s NR 34 R 63 ; —(CH 2 ) m (CHR 61 ) s OCONR 75 R 82 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 78 R 82 ; —(CH 2 ) o (CHR 61 ) s COR 64 ; —(CH 2 ) o (CHR 61 ) s —CONR 58 R 59 , —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 34  is H; lower alkyl; aryl, or aryl-lower alkyl; 
         R 33  and R 34  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 (CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 35  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) p (CHR 61 ) s COOR 57 ; —(CH 2 ) p (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) p CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) p (CHR 61 ) s C 6 H 4 R 8 ; 
         R 36  is H, alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) p (CHR 61 ) s COOR 57 ; —(CH 2 ) p (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) p CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 37  is H; F; Br; Cl; NO 2 ; CF 3 ; lower alkyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 1 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 38  is H; F; Br; Cl; NO 2 ; CF 3 ; alkyl; alkenyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 1 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 39  is H; alkyl; alkenyl; or aryl-lower alkyl; 
         R 40  is H; alkyl; alkenyl; or aryl-lower alkyl; 
         R 41  is H; F; Br; Cl; NO 2 ; CF 3 ; alkyl; alkenyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 1 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH (CH   2 )(CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 42  is H; F; Br; Cl; NO 2 ; CF 3 ; alkyl; alkenyl; —(CH 2 ) p (CHR 61 ) s OR 55 ; —(CH 2 ) p (CHR 1 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 43  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) o (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) o (CHR 61 ) s C 6 H 4 R 8 ; 
         R 44  is alkyl; alkenyl; —(CH 2 ) r (CHR 61 ) s OR 55 ; —(CH 2 ) r (CHR 61 ) s SR 56 ; —(CH) r (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) r (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) r (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) r (CHR 61 ) s COOR 57 ; —(CH 2 ) r (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) r CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) r (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) r (CHR 61 ) s C 6 H 4 R 8 ; 
         R 45  is H; alkyl; alkenyl; —(CH 2 ) o (CHR 61 ) s OR 55 ; —(CH 2 ) o (CHR 61 ) s SR 56 ; —CH 2 ) o (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) o (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) o (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) s (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) s CHR 61 ) s PO(OR 60 ) 2 ; —(CH 2 ) s (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) s (CHR 61 ) s C 6 H 4 R 8 ; 
         R 46  is H; alkyl; alkenyl; or —(CH 2 ) o (CHR 61 ) p C 6 H 4 R 8 ; 
         R 47  is H; alkyl; alkenyl; or —(CH 2 ) o (CHR 61 ) s OR 55 ; 
         R 48  is H; lower alkyl; lower alkenyl; or aryl-lower alkyl; 
         R 49  is H; alkyl; alkenyl; —(CHR 61 ) s COOR 57 ; (CHR 61 ) s CONR 58 R 59 ; (CHR 61 ) s PO(OR 60   2 ; —(CHR 61 ) s SOR 62 ; or —(CHR 61 ) s C 6 H 4 R 8 ; 
         R 50  is H; lower alkyl; or aryl-lower alkyl; 
         R 51  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) p PO(OR 6 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) p (CHR 61 ) s C 6 H 4 R 8 ; 
         R 52  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR61) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) p PO(OR 60 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) p (CHR 61 ) s C 6 H 4 R 8 ; 
         R 53  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s SR 56 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; —(CH 2 ) o (CHR 61 ) p PO(OR 6 ) 2 ; —(CH 2 ) p (CHR 61 ) s SO 2 R 62 ; or —(CH 2 ) p (CHR 61 ) s C 6 H 4 R 8 ; 
         R 54  is H; alkyl; alkenyl; —(CH 2 ) m (CHR 61 ) s OR 55 ; —(CH 2 ) m (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) m (CHR 61 ) s OCONR 33 R 75 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 )COOR 57 ; —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; or —(CH 2 ) o (CHR 1 ) s C 6 H 4 R 8 ; 
         R 55  is H; lower alkyl; lower alkenyl; aryl-lower alkyl; —(CH 2 ) m (CHR 61 ) s OR 57 ; —(CH 2 ) m (CHR 61 ) s NR 34 R 63 ; —(CH 2 ) m (CHR 61 ) s OCONR 75 R 82 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 78 R 82 ; —(CH 2 ) o (CHR 61 ) s —COR 64 ; —(CH 2 ) o (CHR 61 )COOR 57 ; or —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; 
         R 56  is H; lower alkyl; lower alkenyl; aryl-lower alkyl; —(CH 2 ) m (CHR 61 ) s OR 57 ; —(CH 2 ) m (CHR 61 ) s NR 34 R 63 ; —(CH 2 ) m (CHR 61 ) s OCONR 75 R 82 ; —(CH 2 ) m (CHR 61 ) s NR 20 CONR 78 R 82 ; —(CH 2 ) o (CHR 61 ) s —COR 64 ; or —(CH 2 ) o (CHR 61 ) s CONR 58 R 59 ; 
         R 57  is H; lower alkyl; lower alkenyl; aryl lower alkyl; or heteroaryl lower alkyl; 
         R 58  is H; lower alkyl; lower alkenyl; aryl; heteroaryl; aryl-lower alkyl; or heteroaryl-lower alkyl; 
         R 59  is H; lower alkyl; lower alkenyl; aryl; heteroaryl; aryl-lower alkyl; or heteroaryl-lower alkyl; or 
         R 58  and R 59  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 60  is H; lower alkyl; lower alkenyl; aryl; or aryl-lower alkyl; 
         R 61  is alkyl; alkenyl; aryl; heteroaryl; aryl-lower alkyl; heteroaryl-lower alkyl; —(CH 2 ) m OR 55 ; —(CH 2 ) m NR 33 R 34 ; —(CH 2 ) m OCONR 75 R 82 ; —(CH 2 ) m NR 20 CONR 78 R 82 ;  13  (CH 2 ) o COOR 37 ; —(CH 2 ) o NR 58 R 59 ; or —(CH 2 ) o PO(COR 60 ) 2 ; 
         R 62  is lower alkyl; lower alkenyl; aryl, heteroaryl; or aryl-lower alkyl; 
         R 63  is H; lower alkyl; lower alkenyl; aryl, heteroaryl; aryl-lower alkyl; heteroaryl-lower alkyl; —COR 64 ; —COOR 57 ; —CONR 58 R 59 ; —SO 2 R 62 ; or —PO(OR 60 ) 2 ; 
         R 34 and R 63  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 (CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 64  is H; lower alkyl; lower alkenyl; aryl; heteroaryl; aryl-lower alkyl; heteroaryl-lower alkyl; —(CH 2 ) p (CHR 61 ) s OR 65 ; —(CH 2 ) p (CHR 61 ) s SR 66 ; or —(CH 2 ) p (CHR 61   s N 34 R 63 ; —(CH 2 ) P (CHR 61 ) s OCONR 75 R 82 ; —(CH 2 ) P (CHR 61 ) s NR 20 CONR 78 R 82 ; 
         R 65  is H; lower alkyl; lower alkenyl; aryl, aryl-lower alkyl; heteroaryl-lower alkyl; —COR 57 ; —COOR 57 ; or —CONR 58 R 59 ; 
         R 66  is H; lower alkyl; lower alkenyl; aryl; aryl-lower alkyl; heteroaryl-lower alkyl; or —CONR 58 R 59 ; 
         m is 2-4; o is 0-4; p is 1-4; q is 0-2; r is 1 or 2; s is 0 or 1; 
         Z is a chain of n α-amino acid residues, n being the integer 18 and the positions of said amino acid residues in said chain being counted starting from the N-terminal amino acid, 
         whereby these amino acid residues are, depending on their position in the chains, Gly, NMeGly, Pro or Pip, or of formula -A-CO—, or of formula —B—CO—, or of one of the types 
         C: —NR 20 CH(R 72 )CO—; 
         D: —NR 20 CH(R 73 )CO—; 
         E: —NR 20 CH(R 74 )CO—; 
         F: —NR 20 CH(R 84 )CO—; and 
         H: —NR 20 —CH(CO—)—(CH 2 ) 4-7 —CH(CO—)—NR 20 —;
 —NR 20 —CH(CO—)—(CH 2 ) p SS(CH 2 ) p —CH(CO—)—NR 20 —; 
 —NR 20 —CH(CO—)—(—(CH 2 ) p NR 20 CO(CH 2 ) p —CH(CO—)—NR 20 —; and 
 —NR 20 —CH(CO—)—(—(CH 2 ) p NR 20 CONR 20 (CH 2 ) p —CH(CO—)—NR 20 —; 
 
         I: —NR 86 CH 2 CO—; 
         R 71  is lower alkyl; lower alkenyl; —(CH 2 ) p (CHR 61 ) s OR 75 ; —(CH 2 ) p (CHR 61 ) s SR 75 ; —(CH 2 ) p (CHR 61 ) s NR 33 R 34 ; —(CH 2 ) p (CHR 61 ) s OCONR 33 R 75 ; —(CH 2   p (CHR 61 ) s NR 20 CONR 33 R 82 ; —(CH 2 ) o (CHR 61 ) s COOR 75 ; —(CH 2 ) p CONR 58 R 59 ; —(CH 2 ) p PO(OR 62 ) 2 ;  13  (CH 2 ) p SO 2 R 62 ; or —(CH 2 ) o —C 6 R 67 R 68 R 69 R 70 R 76 ; 
         R 72  is H, lower alkyl; lower alkenyl; —(CH 2 ) p (CHR 61 ) s OR 85 ; or —(CH 2 ) p (CHR 61 ) s SR 85 ; 
         R 73  is —(CH 2 ) o R 77 ; —(CH 2 ) r O(CH 2 ) o R 77 ; —(CH 2 ) r S(CH 2 ) o R 77 ; or —(CH 2 ) r NR 20 (CH 2 ) o R 77 ; 
         R 74  is —(CH 2 ) p NR 78 R 79 ; —(CH 2 ) p NR 77 R 80 ; —(CH 2 ) p C(═NR 80 )NR 8 R 79 ; —(CH 2 ) p C(═NOR 50 )NR 78 R 79 ; —(CH 2 ) p C(═NNR 78 R 79 )NR 78 R 79 ; —(CH 2 ) p NR 80 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) p N═C(NR 78 R 80 )NR 79 R 80 ; —(CH 2 ) p C 6 H 4 NR 78 R 79 ; —(CH 2 ) p C 6 H 4 NR 77 R 80 ; —(CH 2 ) p C 6 H 4 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) p C 6 H 4 C(═NOR 50 )NR 78 R 79 ; —(CH 2 ) p C 6 H 4 C(═NNR 78 R 79 )NR 78 R 79 ; —(CH 2 ) p C 6 H 4 NR 80 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) p C 6 H 4 N═C(NR 78 R 80 )NR 79 R 80 ; —(CH 2 ) r O(CH 2 ) m NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) m NR 77 R 80 ; —(CH 2 ) r O(CH 2 ) p C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) p C(═NOR 50 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) p C(═NNR 78 R 79 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) m NR 80 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) m N═C(NR 78 R 80 )NR 79 R 80 ; —(CH 2 ) r O(CH 2 ) p C 6 H 4 CNR 78 R 79 ; —(CH 2 ) r O(CH 2 ) p C 6 H 4 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) p C 6 H 4 C(═NOR 50 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) p C 6 H 4 C(═NNR 78 R 79 )NR 78 R 79 ; —(CH 2 ) r O(CH 2 ) p C 6 H 4 NR 80 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) m NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) m NR 77 R 80 ; —(CH 2 ) r S(CH 2 ) p C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) p C(═NOR 50 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) p C(═NNR 78 R 79 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) m NR 80 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) m N═C(NR 78 R 80 )NR 79 R 80 ; —(CH 2 ) r S(CH 2 ) p C 6 H 4 CNR 78 R 79 ; —(CH 2 ) r S(CH 2 ) p C 6 H 4 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) p C 6 H 4 C(═NOR 50 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) p C 6 H 4 C(═NNR 78 R 79 )NR 78 R 79 ; —(CH 2 ) r S(CH 2 ) p C 6 H 4 NR 80 C(═NR 80 )NR 78 R 79 ; —(CH 2 ) p NR 80 COR 64 ; —(CH 2 ) p NR 80 COR 77 ; —(CH 2 ) p NR 80 CONR 78 R 79 ; —(CH 2 ) p C 6 H 4 NR 80 CONR 78 R 79 ; or —(CH 2 ) p NR 20 CO—[(CH 2 ) u —X] t —CH 3  where X is —O—; —NR 20 —, or —S—; u is 1-3, and t is 1-6; 
         R 75  is lower alkyl; lower alkenyl; or aryl-lower alkyl; 
         R 33  and R 75  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 75  and R 82  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 ; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 76  is H; lower alkyl; lower alkenyl; aryl-lower alkyl; —(CH 2 ) o OR 72 ; —(CH 2 ) o SR 72 ; —(CH 2 ) o NR 33 R 34 ; —(CH 2 ) o OCONR 33 R 75 ; —(CH 2 ) o NR 20 CONR 33 R 82 ; —(CH 2 ) o COOR 75 ; —(CH 2 ) o CONR 58 R 59 ; —(CH 2 ) o PO(OR 60 ) 2 ; —(CH 2 ) p SO 2 R 62 ; or —(CH 2 ) o COR 64 ; 
         R 77  is a heteroaryl group of one of the formulae 
       
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         R 78  is H; lower alkyl; aryl; or aryl-lower alkyl; 
         R 78  and R 82  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 79  is H; lower alkyl; aryl; or aryl-lower alkyl; or 
         R 78  and R 79 , taken together, can be —(CH 2 ) 2-7 —; —(CH 2 ) 2 O(CH 2 ) 2 ; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 80  is H; or lower alkyl; 
         R 81  is H; lower alkyl; or aryl-lower alkyl; 
         R 82  is H; lower alkyl; aryl; heteroaryl; or aryl-lower alkyl; 
         R 33  and R 82  taken together can form: —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; 
         R 83  is H; lower alkyl; aryl; or —NR 78 R 79 ; 
         R 84  is —(CH 2 ) m (CHR 61 ) s OH; —(CH 2 )pCOOR 80 ; —(CH 2 ) m (CHR 61 ) s SH; —(CH 2 ) p CONR 78 R 79 ; —(CH 2 ) p NR 80 CONR 78 R 79 ; —(CH 2 ) p C 6 H 4 CONR 78 R 79 ; or —(CH 2 ) p C 6 H 4 NR 80 CONR 78 R 79 ; 
         R 85  is lower alkyl; or lower alkenyl; 
         R 86  is R 74 ; —(CH 2 ) o R 77 ; —(CH 2 ) o —CHR 33 R 75 ; or —[(CH 2 ) u —X′] t —(CH 2 ) v NR 78 R 79 ; or —[(CH 2 ) u —X′] t —(CH 2 ) v —C(═NR 80 )NR 78 R 79  where X is —O—, —NR 20 —, —S—; or —OCOO—, u is 1-3, t is 1-6, and v is 1-3; 
         with the proviso that
 the amino acid residues in positions 1 to 18 are: 
 P1: of type D or of type E or of type C, or of the type F; 
 P2: of type E, or of type F, or of type D; 
 P3: or of type C, of type D; 
 P4: of type E, or of type D, or of type F; 
 P5: of type D, or of type C, or of type E; 
 P6: of type C, or of type E, or of type F; 
 P7: of type C, or of type D, or of type E or of type F; 
 P8: of type F, or of type E, or the residue is Gly or NMeGly; 
 P9: of type C, or of type D, or of type F; 
 P10: of type C, or of type E, or of formula -A-CO—, or the residue is Pro or Pip; 
 P11: of type C, or of type E, or of formula —B—CO—, or the residue is Gly, NMeGly, Pro or Pip; 
 P12: of type D, or of type C, or of type F; 
 P13: of type E, or of type F, or the residue is Gly or NMeGly; 
 P14: of type C, or of type D, or of type F; 
 P15: of type E, or of type F; 
 P16: of type D, or of type E, or of type F; 
 P17: of type E, or of type F, and; 
 P18: of type C, or of type D, or of type E, or of type F; or 
 P4 and P17 and/or P6 and P15 and/or P8 and P13, taken together, can form a group of type H; 
 at P10, P11 and P12 also D-isomers being possible; 
 
         and pharmaceutically acceptable salts thereof. 
       
     
     
       2. A compound according to  claim 1  wherein 
       
         
           
           
               
               
           
         
       
       is a group of formula (a1) or (a2). 
     
     
       3. A compound according to  claim 2  wherein A is a group of one of the formulae A1 to A69;
 R 1  is hydrogen or lower alkyl; 
 R 2  is H; lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —CH 2 ) m SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64 (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); (CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is Lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 3  is H; lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) m SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is Lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 4  is H; lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) m SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64 (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57 : is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 5  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); (CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 2 ° is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is alkyl; alkenyl; aryl; aryl-lower alkyl; or heteroaryl-lower alkyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or Lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 6  is H; lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR  20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 )O(CH 2 ) 2 ; —(CH 2 ) 2 S(CH 2 ) 2 —; or (CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 7  is lower alkyl; lower alkenyl; —(CH 2 ) q OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) q SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) q NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) q OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —l ; where R 57  is H; or lower alkyl); —(CH 2 ) q NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) q N(R 20 COR 64 (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) r COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) q CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) r PO(OR 60 ) 2  where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) r SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 8  is H; F; Cl; lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —l ; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 COR 64 (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) r COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) r PO(OR 60 ) 2  where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) r SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 9  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl);—(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 10  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64 (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 11  is H; lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57 : H is or lower alkyl); —(CH 2 ) o NR  20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64 (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 12  is H; lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) m SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64  (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) r COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) r PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 13  is lower alkyl; lower alkenyl; —(CH 2 ) q OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) q SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) q NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) q OCONR 33 R 75  (where R 33 is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —, where R 57  is H; or lower alkyl); —(CH 2 ) q NR  20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) r COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) r CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) r PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) r SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy): 
 R 14  is lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) q SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) q NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) q N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) r COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) q CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) r PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 15  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl is R 82 : H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl);—CH 2 ) o N(R 20 )COR 64  (where R 20  is H; lower alkyl; R 64  is lower alkyl; or lower alkenyl); —NR 20 CO lower alkyl (R 20 −H; or lower alkyl; —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or (CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 16  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR  20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or (CH 2 ) q C 6 H 4 R 8 (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); and 
 R 17  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) q NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) q N(R 20 )COR 64  (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) r COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) r PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) r SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy). 
 
     
     
       4. A compound according to  claim 2  wherein A is a group of one of the formulae A5 (with R 2  being H); A8; A22; A25; A38 (with R 2  being H); A42; and A50. 
     
     
       5. A compound according to  claim 4  wherein A is a group of formula 
       
         
           
           
               
               
           
         
       
       wherein R 20  is H or lower alkyl; and R 64  is alkyl; alkenyl; —[(CH 2 ) u —X] t —CH 3 , wherein X is —O—; —NR 20 —, —S—; u=1-3, t=1-6, aryl; aryl-lower alkyl; or heteroaryl-lower alkyl. 
     
     
       6. A compounds according to  claim 5  wherein R 64  is n-hexyl; n-heptyl; 4-(phenyl)benzyl; diphenylmethyl, 3-amino-propyl; 5-amino-pentyl; methyl; ethyl; isopropyl; isobutyl; n-propyl; cyclohexyl; cyclohexylmethyl; n-butyl; phenyl; benzyl; (3-indolyl)methyl; 2-(3-indolyl)ethyl; (4-phenyl)phenyl; n-nonyl; CH 3 —OCH 2 CH 2 —OCH 2 — or CH 3 —(OCH 2 CH 2 ) 2 )—OCH 2 —. 
     
     
       7. A compound according to  claim 2  wherein A is a group of one of the formulae A70 to A104;
 R 20  is H; or lower alkyl; 
 R 18  is lower alkyl; 
 R 19  is lower alkyl; lower alkenyl; —(CH 2 ) p OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) p SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) p NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); (CH 2 ) p COOR 57  (where R 57 : lower alkyl; or lower alkenyl); (CH 2 ) p CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; or lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) p SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or (CH 2 ) o C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 21  is H; lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33  R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 22  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); (CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); -(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64 (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 23  is H; lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 —; where R 57  is H; or lower alkyl); -(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —NR 20 CO lower alkyl (R 20 ═H; or lower alkyl) —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 24  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —NR 20 CO lower alkyl (R 20 ═H ; or lower alkyl) —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 )—; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 25  is H; lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33  R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 26  is H; lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or (CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); or, alternatively, R 25  and R 26  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 34 (CH 2 ) 2 —; 
 R 27  is H; lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64  (where R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60  ) 2 (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); 
 R 28  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64 (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); and 
 R 29  is lower alkyl; lower alkenyl; —(CH 2 ) o OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) o SR 56  (where R 56  is lower alkyl; or lower alkenyl); —(CH 2 ) o NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o N(R 20 )COR 64 (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —NR 20 CO lower-alkyl (R 20 ═H; or lower alkyl) —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy). 
 
     
     
       8. A compound according to  claim 7  wherein R 23 , R 24  and R 29  are —NR 20 —CO-lower alkyl where R 20  is H; or lower alkyl. 
     
     
       9. A compound according to  claim 7  wherein A is a group of one of the formulae A74 (with R 22  being H); a75; A76; A77 (with R 22  being H); A78; and A79. 
     
     
       10. A compound according to  claim 2  wherein B is a group of formula —NR 20 CH(R 71 )— or an enantiomer of one of the groups A5 (with R 2  being H); A8; A22; A25; A38 (with R 2  being H); A42; A47; and A50. 
     
     
       11. A compound according to  claim 10  wherein B—CO is Ala; Arg; Asn; Cys; Gln; Gly; His; Ile; Leu; Lys; Met; Phe; Pro; Ser; Thr; Trp; Tyr; Val; Cit; Orn; tBuA; Sar; t-BuG; 4AmPhe; 3AmPhe; 2AmPhe; Phe(mC(NH 2 )═NH; Phe(pC(NH 2 )═NH; Phe(mNHC (NH 2 )═NH; Phe(pNHC (NH 2 )═NH; Phg; Cha; cyclobutylalanine; cyclopentyalanine; Nle; 2-Nal; 1-Nal; 4Cl-Phe; 3Cl-Phe; 2Cl-Phe; 3,4Cl 2 Phe; 4F-Phe; 3F-Phe; 2F-Phe; Tic; Thi; Tza; Mso; AcLys; Dpr; A 2 Bu; Dbu; Abu; Aha; Aib; Y(Bzl); Bip; S(Bzl); T(Bzl); hCha; hCys; hSer, hArg; hPhe; Bpa; Pip; OctG; MePhe; MeNle; MeAla; MeIle; MeVal; or MeLeu. 
     
     
       12. A compound according to  claim 10  wherein B is a group, having (L)-configuration, of formula 
       
         
           
           
               
               
           
         
       
       wherein R 20  is H; or lower alkyl; and R 64  is alkyl; alkenyl; —[(CH 2 ) u —X] t —CH 3 , wherein X is —O—, —NR 20 —, —S—; u=1-3, t=1-6; aryl; aryl-lower alkyl; or heteroaryl-lower alkyl. 
     
     
       13. A compound according to  claim 12  wherein R 64  is n-hexyl; n-heptyl; 4-(phenyl)benzyl; diphenylmethyl, 3-amino-propyl; 5-amino-pentyl; methyl; ethyl; isopropyl; isobutyl; n-propyl; cyclohexyl; cyclohexylmethyl; n-butyl; phenyl; benzyl; (3-indolyl)methyl; 2-(3-indolyl)ethyl; (4-phenyl)phenyl; n-nonyl; CH 3 —OCH 2 CH 2 —OCH 2 — or CH 3 —(OCH 2 CH 2 ) 2 —OCH 2 —. 
     
     
       14. A compound according to  claim 1  wherein 
       
         
           
           
               
               
           
         
       
       is a group of formula (b1)) or (1);
 R 1  is H; or lower alkyl; 
 R 20  is H; or lower alkyl; 
 R 30  is H; or methyl; 
 R 31  is H; lower alkyl; lower alkenyl; —(CH 2 ) p OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) p NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) r C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); most preferably —CH 2 CONR 58 R 59  (where R 58  is H; or lower alkyl; and R 59  is lower alkyl; or lower alkenyl); 
 R 32  is H; or methyl; 
 R 33  is lower alkyl; lower alkenyl; —(CH 2 ) m OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) m NR 34 R 63  (where R 34  is lower alkyl; or lower alkenyl; R 63  is H; or lower alkyl; or R 34  and R 63  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 75 R 82  (where R 75  is lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 75  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 78 R 82  (where R 20  is H; or lower alkyl; R 78  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 78  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57 : H; or lower alkyl); 
 R 34  is H; or lower alkyl; 
 R 35 : is H; lower alkyl; lower alkenyl; (CH 2 ) m OR 55  (where R 55 : lower alkyl; or lower alkenyl); —(CH 2 ) m NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —CH 2   2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) m N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl; or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); 
 R 36 : lower alkyl; lower alkenyl; or aryl-lower alkyl; 
 R 37  is H; lower alkyl; lower alkenyl; —(CH 2 ) p OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) p NR 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p NR 20 CONR 33 R 82  where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p N(R 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —CH) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy); and 
 R 38  is H; lower alkyl; lower alkenyl; —(CH 2 ) p OR 55  (where R 55  is lower alkyl; or lower alkenyl); —(CH 2 ) p R 33 R 34  (where R 33  is lower alkyl; or lower alkenyl; R 34  is H; or lower alkyl; or R 33  and R 34  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p OCONR 33 R 75  (where R 33  is H; or lower alkyl; or lower alkenyl; R 75  is lower alkyl; or R 33  and R 75  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p NR 20 CONR 33 R 82  (where R 20  is H; or lower alkyl; R 33  is H; or lower alkyl; or lower alkenyl; R 82  is H; or lower alkyl; or R 33  and R 82  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) p N(R) 20 )COR 64  (where: R 20  is H; or lower alkyl; R 64  is lower alkyl; or lower alkenyl); —(CH 2 ) o COOR 57  (where R 57  is lower alkyl; or lower alkenyl); —(CH 2 ) o CONR 58 R 59  (where R 58  is lower alkyl, or lower alkenyl; and R 59  is H; lower alkyl; or R 58  and R 59  taken together are —(CH 2 ) 2-6 —; —(CH 2 ) 2 O(CH 2 ) 2 —; —(CH 2 ) 2 S(CH 2 ) 2 —; or —(CH 2 ) 2 NR 57 (CH 2 ) 2 —; where R 57  is H; or lower alkyl); —(CH 2 ) o PO(OR 60 ) 2  (where R 60  is lower alkyl; or lower alkenyl); —(CH 2 ) o SO 2 R 62  (where R 62  is lower alkyl; or lower alkenyl); or —(CH 2 ) q C 6 H 4 R 8  (where R 8  is H; F; Cl; CF 3 ; lower alkyl; lower alkenyl; or lower alkoxy). 
 
     
     
       15. A compound according to  claim 14  wherein R 1  is H; R 20  is H; R 30  is H; R 31  carboxymethyl; or lower alkoxycarbonylmethyl; R 32  is H; R 35  is methyl; R 36  is methoxy; R 37  is H and R 38  is H. 
     
     
       16. A compound according to  claim 1  wherein the α-amino acid residues in position 1 to 18 are:
 P1: of type D, or of type E; 
 P2: of type E, or of type F; 
 P3: of type C, or of type D; 
 P4: of type E, or of type F; 
 P5: of type D, or of type E; 
 P6: of type E, or of type F; 
 P7: of type E, or of type F; 
 P8: of type E, or of type F, or the residue is Gly or NMeGly; 
 P9: of type D; 
 P10: of type E, or of formula -A1-A69-CO—, or the residue is Pro or Pip; 
 P11: of type E, or of formula —B—CO—, or the residue is Gly, NMeGly, Pro or Pip; 
 P12: of type D; 
 P13: of type F, or of type E, or the residue is Gly or NMeGly; 
 P14: of type C, or of type D; 
 P15: of type E, or of type F; 
 P16: of type E or of type F; 
 P17: of type E, or of type F; and 
 P18: of Type C or of type D or of type E or of Type F; or 
 P4 and P17 and/or P6 and P15 and/or P8 and P13, taken together, form a group of type H; 
 at P10, P11 and P12 also D-isomers being possible. 
 
     
     
       17. A compound according to  claim 16  wherein the α-amino acid residues in positions 1 to 18 are:
 P1: Arg; 
 P2: Arg; 
 P3: 2-Nal, Tip, Tyr; 
 P4: Cys; 
 P5: Tyr; 
 P6: Cit, Gln, Arg; 
 P7: Lys; 
 P8: Cys, Gly; 
 P9: Tyr; 
 P10: Lys,  D Lys,  D Pro; 
 P11: Gly, Pro,  D Pro; 
 P12: Tyr; 
 P13: Cys, Gly; 
 P14: Tyr; 
 P15: Arg; 
 P16: Cit, Thr, Lys; 
 P17: Cys; and 
 P18: Arg; or 
 Cys at P4 and P17 and/or at P8 and P13 form a disulfide bridge. 
 
     
     
       18. A compound of formula I according to  claim 1  wherein the template is Gly- D Pro, and the amino acid residues in position 1-18 are:
 P1: Arg; 
 P2: Arg; 
 P3: Trp; 
 P4: Cys; 
 P5: Tyr; 
 P6: Arg; 
 P7: Lys; 
 P8 Cys; 
 P9: Tyr; 
 P10: Lys; 
 P11: Gly; 
 P12: Tyr; 
 P13: Cys; 
 P14: Tyr; 
 P15: Arg; 
 P16: Lys; 
 P17: Cys; and 
 P18: Arg 
 Cys at P4 and P17 and at P8 and P13 forming disulfide bridges. 
 
     
     
       19. A compound of formula I as defined in  claim 1 , further including enantiomers of said compound of formula I. 
     
     
       20. A compound according to  claim 1  having CXCR4 antagonizing activity, which also has anticancer activity and/or anti inflammatory activity, wherein the cancer is selected from the group consisting of breast cancer, brain cancer, prostate cancer, lung cancer, kidney cancer, neuroblastoma, non-hodgkin&#39;s lymphoma, ovarian cancer, multiple myeloma, chronic lymphocytic leukemia, pancreatic cancer, melanoma, and whereas the inflammatory activity is selected from the group consisting of asthma, allergic rhinitis, hypersensitivity lung diseases, hypersensitivity pneumonitis, eosinophilic pneumonias, delayed-type hypersensitivity, interstitial lung disease (ILD), idiopathic pulmonary fibrosis, ILD associated with rheumatoid arthritis, systemic lupus erythematosus, ankylosing sponylitis, systemic sclerosis, Sjogren&#39;s syndrome, systemic anaphylaxis or hypersensitivity responses, drug allergies, rheumatoid arthritis, psoriatic arthritis, systemic lupus erythematosus, myasthenia gravis, juvenile onset diabetes, glomerulonephritis, autoimmune thyroiditis, graft rejection including allograft rejection or graft-versus-host disease, inflammatory bowel diseases and inflammatory dermatoses. 
     
     
       21. A pharmaceutical composition containing a compound according to  claim 1  and a pharmaceutically inert carrier. 
     
     
       22. A composition according to  claim 21  in a form suitable for oral, topical, transdermal, injection, buccal, transmucosal, pulmonary or inhalation administration. 
     
     
       23. A composition according to  claim 21  in form of tablets, dragees, capsules, solutions, liquids, gels, plaster, creams, ointments, syrup, slurries, suspensions, spray, nebuliser or suppositories. 
     
     
       24. A method of antagonizing CXCR4 in a patient in need thereof, comprising administering to the patient an effective amount of a compound according to  claim 1 . 
     
     
       25. The method according to  claim 24  wherein said antagonism of CXCR4 is intended to be for slowing viral progression in infected patients. 
     
     
       26. A process for the manufacture of compounds according to  claim 1  which process comprises
 (a) coupling an appropriately functionalized solid support with an appropriately N-protected derivative of that amino acid which in the end-product is in position 8, 9 or 10 , any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
 (b) removing the N-protecting group from the product thus obtained; 
 (c) coupling the product thus obtained with an appropriately N-protected derivative of that amino acid which is one position nearer the N-terminal amino acid residue, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
 (d) removing the N-protecting group from the product thus obtained; 
 (e) repeating steps (c) and (d) until the N-terminal amino acid residue has been introduced; 
 (f) coupling the product thus obtained with a compound of the general formula 
 
       
         
           
           
               
               
           
         
         wherein 
       
       
         
           
           
               
               
           
         
         is as defined in  claim 1  and X is an N-protecting group or, alternatively, if 
       
       
         
           
           
               
               
           
         
         is to be group (a1) or (a2), above,
 (fa) coupling the product obtained in step (e) with an appropriately N-protected derivative of an amino acid of the general formula
   HOOC—B—H   III
 
   or 
   HOOC-A-H   IV
 
 
 wherein B and A are as defined in  claim 1 , any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
 (fb) removing the N-protecting group from the product thus obtained; and 
 (fc) coupling the product thus obtained with an appropriately N-protected derivative of an amino acid of the above general formula IV and, respectively, III, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; and, respectively, if 
 
       
       
         
           
           
               
               
           
         
         
           is to be group (a3), above, 
           (fa′) coupling the product obtained in step (e) with an appropriately N-protected derivative of an amino acid of the above general formula III, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
           (fb′) removing the N-protecting group from the product thus obtained; and 
           (fc′) coupling the product thus obtained with an appropriately N-protected derivative of an amino acid of the above general formula III, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
         
         (g) removing the N-protecting group from the product obtained in step (f) or (fc) or (fc′); 
         (h) coupling the product thus obtained with an appropriately N-protected derivative of that amino acid which is in position 18 if n is18, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
         (i) removing the N-protecting group from the product thus obtained; 
         (j) coupling the product thus obtained with an appropriately N-protected derivative of that amino acid which is one position farther away from position 18 if n is 18, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
         (k) removing the N-protecting group from the product thus obtained; 
         (l) repeating steps (j) and (k) until all amino acid residues have been introduced; 
         (m) optionally, selectively deprotecting one or several protected functional group(s) present in the molecule and appropriately substituting the reactive group(s) thus liberated; 
         (n) optionally, forming one, two or three interstrand linkage(s) between side-chains of appropriate amino acid residues at opposite positions of the β-strand region; 
         (o) detaching the product thus obtained from the solid support; 
         (p) cyclizing the product cleaved from the solid support; 
         (q) removing any protecting groups present on functional groups of any members of the chain of amino acid residues and, optionally, any protecting group(s) which may in addition be present in the molecule; and 
         (r) if desired, converting the product thus obtained into a pharmaceutically acceptable salt or converting a pharmaceutically acceptable, or unacceptable, salt thus obtained into the corresponding free compound of formula I or into a different, pharmaceutically acceptable, salt. 
       
     
     
       27. A process for the manufacture of compounds according to  claim 1  which process comprises
 (a′) coupling an appropriately functionalized solid support with a compound of the general formula 
 
       
         
           
           
               
               
           
         
         wherein 
       
       
         
           
           
               
               
           
         
         is as defined above and X is an N-protecting group or, alternatively, if 
       
       
         
           
           
               
               
           
         
         is to be group (al) or (a2), above,
 (a′a) coupling said appropriately functionalized solid support with an appropriately N-protected derivative of an amino acid of the general formula
   HOOC—B—H   III
 
   or 
   HOOC-A-H   IV
 
 
 wherein B and A are as defined in  claim 1 , any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
 (a′b) removing the N-protecting group from the product thus obtained; and 
 (a′c) coupling the product thus obtained with an appropriately N-protected derivative of an amino acid of the above general formula IV and, respectively, III, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; and, respectively, if 
 
       
       
         
           
           
               
               
           
         
         
           is to be group (a3), above, 
           (a′a′) coupling the product obtained in step (e) with an appropriately N-protected derivative of an amino acid of the above general formula III, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
           (a′b′) removing the N-protecting group from the product thus obtained; and 
           (a′c′) coupling the product thus obtained with an appropriately N-protected derivative of an amino acid of the above general formula III, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
         
         (b′) removing the N-protecting group from the product obtained in step (a′), (a′c) or (a′c′); 
         (c′) coupling the product thus obtained with an appropriately N-protected derivative of that amino acid in position 18 if n is 18, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
         (d′) removing the N-protecting group from the product thus obtained; 
         (e′) coupling the product thus obtained with an appropriately N-protected derivative of that amino acid which is one position farther away from position 18 if n is 18, any functional group which may be present in said N-protected amino acid derivative being likewise appropriately protected; 
         (f′) removing the N-protecting group from the product thus obtained; 
         (g′) repeating steps (e′) and (f′) until all amino acid residues have been introduced; 
         (h′) optionally, selectively deprotecting one or several protected functional group(s) present in the molecule and appropriately substituting the reactive group(s) thus liberated; 
         (i′) optionally forming one, two or three interstrand linkage(s) between side-chains of appropriate amino acid residues at opposite positions of the β-strand region; 
         (j′) detaching the product thus obtained from the solid support; 
         (k′) cyclizing the product cleaved from the solid support; 
         (l′) removing any protecting groups present on functional groups of any members of the chain of amino acid residues and, optionally, any protecting group(s) which may in addition be present in the molecule; and 
         (m′) optionally, converting the product thus obtained into a pharmaceutically acceptable salt or converting a pharmaceutically acceptable, or unacceptable, salt thus obtained into the corresponding free compound of formula I or into a different, pharmaceutically acceptable, salt. 
       
     
     
       28. A process according to  claim 26  but wherein N-substituted glycine derivatives are introduced by coupling with a leaving group-containing acylating agent, followed by nucleophilic displacement with an amine of the formula H 2 N—R 86  which, if necessary, is appropriately protected. 
     
     
       29. A process according to  claim 28  wherein said leaving group-containing acylating agent is bromo, chloro or iodo acetic acid. 
     
     
       30. The process according to  claim 26  wherein the process is modified for the manufacture of enantiomers of the compound in which enantiomers of all chiral starting materials are used. 
     
     
       31. A process according to  claim 27 , but wherein an amino acid residue of type I is introduced by coupling with a leaving group-containing acylating agent, followed by nucleophilic displacement with an amine of the formula H 2 N—R 86  which, if necessary, is appropriately protected. 
     
     
       32. A process according to  claim 27  wherein the process is modified for the manufacture of enantiomers of the compounds in which enantiomers of all chiral starting materials are used. 
     
     
       33. A process according to  claim 28  wherein the process is modified for the manufacture of enantiomers of the compounds in which enantiomers of all chiral starting materials are used. 
     
     
       34. A process according to  claim 29  wherein the process is modified for the manufacture of enantiomers of the compounds in which enantiomers of all chiral starting materials are used. 
     
     
       35. A compound according to  claim 1  wherein the template is Gly- D Pro, and the amino acid residues in position 1-18 are:
 P1: Arg; 
 P2: Arg; 
 P3: Trp; 
 P4: Cys; 
 P5: Tyr; 
 P6: Gln; 
 P7: Lys; 
 P8: Cys; 
 P9: Tyr; 
 P10: Lys; 
 P11: Gly; 
 P12: Tyr; 
 P13: Cys; 
 P14: Tyr; 
 P15: Arg; 
 P16: Cit; 
 P17: Cys; and 
 P18: Arg 
 Cys at P4 and P17 and at P8 and P13 forming a disulfide bridge.
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